GPBAR-A

Cat. No. 4478 2 Citations Submit a Review Datasheet / COA / SDS

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Description: GPBA receptor (TGR5) agonist

Chemical Name: 4-[[3,5-Bis(trifluoromethyl)phenyl]methyl]-6-(2-fluorophenyl)-4,5-dihydro-pyrido[3,2-f]-1,4-oxazepin-3(2H)-one

Purity: ≥98% (HPLC)

Datasheet

Citations (2)

Reviews

Pathways (1)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for GPBAR-A

GPBAR-A is a gPBA receptor agonist. Upregulates GLP-1 secretion from intestinal cultures. Increases MQAE-fluorescence suggesting a decrease in intracellular chloride concentration in gallbladder epithelial cells.

Technical Data for GPBAR-A

M. Wt	484.37
Formula	C₂₃H₁₅F₇N₂O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	877052-79-4
PubChem ID	11656002
InChI Key	ZIXNJVGTAXRKAP-UHFFFAOYSA-N
Smiles	O=C(CO3)N(CC4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)CC1=C3N=CC=C1C2=C(F)C=CC=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GPBAR-A

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	48.44	100
	ethanol	9.69	20

Preparing Stock Solutions for GPBAR-A

The following data is based on the product molecular weight 484.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.06 mL	10.32 mL	20.65 mL
5 mM	0.41 mL	2.06 mL	4.13 mL
10 mM	0.21 mL	1.03 mL	2.06 mL
50 mM	0.04 mL	0.21 mL	0.41 mL

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Product Datasheets for GPBAR-A

Certificate of Analysis / Product Datasheet

Safety Datasheet

References for GPBAR-A

References are publications that support the biological activity of the product.

Parker et al (2012) Molecular mechanisms underlying bile acid-stimulated glucagon-like peptide-1 secretion. Br.J.Pharmacol. 165 414 PMID: 21718300

Keitel et al (2009) The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders. Hepatology 50 861 PMID: 19582812

If you know of a relevant reference for GPBAR-A, please let us know.

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Keywords: GPBAR-A, GPBAR-A supplier, TGR5, agonists, g-protein, bile, acid, receptors, GPBA, GPBAR, Receptors, 4478, Tocris Bioscience

2 Citations for GPBAR-A

Citations are publications that use Tocris products. Selected citations for GPBAR-A include:

Kowal et al (2015) Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells. Stem Cells Transl Med 13 28 PMID: 26050734

Bas et al (2021) A turquoise fluorescence lifetime-based biosensor for quantitative imaging of intracellular calcium. Nat Commun 12 7159 PMID: 34887382

Do you know of a great paper that uses GPBAR-A from Tocris? Please let us know.

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Pathways for GPBAR-A

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.